AICAR inhibits the growth of EGFR-activated cancer cell lines, including glioblastoma cells. (A) Western blot analysis demonstrated Akt Ser-473 phosphorylation in U87-EGFRvIII, but not U87 cells in response to rapamycin (1 nM) for 24 h. (B) Immunoblot analysis of effect of AICAR (0.5 mM) on Akt and mTORC1 signaling. U87-EGFRvIII cells were treated for up to 24 h and effect on signaling pathways was determined at indicated time points. AICAR (0.5 mM) treatment for up to 24 h inhibited mTOR signaling (S6K and S6 phosphorylation), but does not induce Akt phosphorylation. AICAR also phosphorylated AMPK downstream target gene ACC. (C) U87, U87-EGFRvIII, and U87-EGFR glioblastoma cells were seeded in 96-well plates for 24 h and then treated for 3 days with AICAR at the doses indicated. Relative growth was measured using the WST assay (Chemicon). AICAR was significantly more effective at blocking the growth of wild-type EGFR or EGFRvIII- expressing glioblastoma cells, relative to their parental U87 counterparts (*, P < 0.05; #, P < 0.05). (D) AICAR (0.5 mM) was more effective than rapamycin (Rapa 1 nM) in blocking the growth of cancer cells with activated EGFR signaling. Cell lines were treated with indicated drugs for 3 days, and cell number was determined by trypan exclusion. EGFR level of cell line is U87 (low expression), U87/EGFR (high expression), U87/EGFRvIII (high expression/mutation), T98 (high expression), A431 (amplification), and H1975 (L858R1/T790M mutation); cancer cell line type is indicated below the graph. Control cells were treated with ethanol, the diluent, alone (1:1,000).